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Drugs 2002Olmesartan medoxomil is a nonpeptide angiotensin II receptor antagonist which selectively and competitively inhibits the type 1 angiotensin II receptor without affecting... (Review)
Review
Olmesartan medoxomil is a nonpeptide angiotensin II receptor antagonist which selectively and competitively inhibits the type 1 angiotensin II receptor without affecting other receptors regulating the cardiovascular system. In well designed randomised trials, olmesartan medoxomil was significantly more effective than placebo, and at dosages of 10 to 20 mg/day was at least as effective as atenolol 50 to 100 mg/day in reducing diastolic blood pressure (DBP). At dosages of 5 to 20 mg/day, olmesartan medoxomil was more effective than captopril 12.5 to 50mg twice daily at lowering seated DBP in patients with mild to moderate hypertension in a dose titration study. Reductions in seated DBP were greater with olmesartan medoxomil 10 to 20 mg/day than losartan 50 to 100 mg/day. Olmesartan medoxomil at 20 mg/day was more effective in lowering seated DBP than losartan 50 mg/day, valsartan 80 mg/day or irbesartan 150 mg/day, and was more efficacious than losartan 50 mg/day or valsartan 80 mg/day at reducing 24-hour ambulatory systolic blood pressure. Olmesartan medoxomil has shown no clinically important pharmacokinetic interactions with digoxin, warfarin or antacid (aluminium magnesium hydroxide). Adverse events were infrequent in clinical studies of olmesartan medoxomil and were similar to those attributed to placebo. With olmesartan medoxomil, the frequency of dizziness was higher than with placebo but similar to that occurring with losartan, valsartan and irbesartan.
Topics: Angiotensin II; Angiotensin Receptor Antagonists; Animals; Antihypertensive Agents; Humans; Imidazoles; Olmesartan Medoxomil; Randomized Controlled Trials as Topic; Tetrazoles
PubMed: 12076183
DOI: 10.2165/00003495-200262090-00005 -
Drugs 2009black triangle Olmesartan medoxomil/amlodipine is a fixed-dose combination of olmesartan medoxomil and amlodipine, both established antihypertensive agents. Dose... (Review)
Review
black triangle Olmesartan medoxomil/amlodipine is a fixed-dose combination of olmesartan medoxomil and amlodipine, both established antihypertensive agents. Dose titration with the individual constituent drugs is recommended before switching to the equivalent fixed-dose combination. black triangle In a randomized, double-blind, factorial trial in patients with mild to severe hypertension, 8 weeks of olmesartan medoxomil/amlodipine was more effective in reducing diastolic BP (DBP) and systolic BP (SBP) than placebo or equivalent dosages of olmesartan medoxomil or amlodipine as monotherapy. black triangle In two randomized, double-blind trials in patients with moderate to severe hypertension not adequately treated with amlodipine or olmesartan medoxomil monotherapy, 8 weeks of olmesartan medoxomil/amlodipine 20 mg/5 mg, 40 mg/5 mg or 40 mg/10 mg per day was more effective in reducing DBP and SBP than continuing treatment with olmesartan medoxomil 20 mg/day or amlodipine 5 mg/day monotherapy. black triangle More patients receiving olmesartan medoxomil/amlodipine at approved dosages than monotherapy recipients at equivalent dosages reached BP goals (42.5-51.0% vs 21.1-36.3% in the factorial trial and 44.5-54% vs 28.5-30% in the monotherapy comparisons). black triangle In the comparison with amlodipine monotherapy, >70% of olmesartan medoxomil/amlodipine recipients, some requiring upwards dosage adjustment, met BP goals. black triangle Olmesartan medoxomil/amlodipine was generally well tolerated in clinical trials. Peripheral oedema was significantly less common in olmesartan medoxomil/amlodipine 40 mg/10 mg per day than amlodipine monotherapy 10 mg/day recipients.
Topics: Amlodipine; Antihypertensive Agents; Drug Combinations; Humans; Hypertension; Imidazoles; Olmesartan Medoxomil; Randomized Controlled Trials as Topic; Tetrazoles; Treatment Outcome
PubMed: 19405551
DOI: 10.2165/00003495-200969060-00005 -
Drugs 2008Olmesartan medoxomil (Olmetec, Benicar) is an angiotensin II type 1 (AT(1)) receptor antagonist (angiotensin receptor blocker [ARB]) that inhibits the actions of... (Review)
Review
Olmesartan medoxomil (Olmetec, Benicar) is an angiotensin II type 1 (AT(1)) receptor antagonist (angiotensin receptor blocker [ARB]) that inhibits the actions of angiotensin II on the renin-angiotensin-aldosterone system, which plays a key role in the pathogenesis of hypertension. Oral olmesartan medoxomil 10-40 mg once daily is recommended for the treatment of adult patients with hypertension. In those with inadequate BP control using monotherapy, fixed-dose olmesartan medoxomil/hydrochlorothiazide (HCTZ) [Olmetec plus, Benicar-HCT] combination therapy may be initiated. Extensive clinical evidence from several large well designed trials and the clinical practice setting has confirmed the antihypertensive efficacy and good tolerability profile of oral olmesartan medoxomil, as monotherapy or in combination with HCTZ, in patients with hypertension, including elderly patients with isolated systolic hypertension (ISH). Notably, BP control is sustained throughout the 24-hour dosage interval, including during the last 4 hours of this period. In clinical trials, olmesartan medoxomil monotherapy provided better antihypertensive efficacy than losartan, candesartan cilexetil or irbesartan monotherapy, and was at least as effective as valsartan treatment, with a faster onset of action than other ARBs in terms of reductions from baseline in diastolic BP (DBP) and, in most instances, systolic BP (SBP). Combination therapy with olmesartan medoxomil plus HCTZ was superior to that with benazepril plus amlodipine, as effective as that with losartan plus HCTZ, noninferior to that with atenolol plus HCTZ, but less effective than that with telmisartan plus HCTZ, in individual trials. Data from ongoing clinical outcome trials are required to more fully determine the relative position of olmesartan medoxomil therapy in the management of hypertension. In the meantime, the consistent antihypertensive efficacy during the entire 24-hour dosage interval and good tolerability profile of olmesartan medoxomil, with or without HCTZ, make it a valuable option for the treatment of adult patients with hypertension, including the elderly.
Topics: Adult; Aged; Angiotensin II Type 1 Receptor Blockers; Antihypertensive Agents; Diuretics; Drug Combinations; Drug Therapy, Combination; Humans; Hydrochlorothiazide; Hypertension; Imidazoles; Olmesartan Medoxomil; Tetrazoles
PubMed: 18547134
DOI: 10.2165/00003495-200868090-00005 -
Drugs Jan 2011The antihypertensive agents olmesartan medoxomil, amlodipine and hydrochlorothiazide (HCTZ) are now available as a fixed-dose combination tablet (olmesartan... (Review)
Review
The antihypertensive agents olmesartan medoxomil, amlodipine and hydrochlorothiazide (HCTZ) are now available as a fixed-dose combination tablet (olmesartan medoxomil/amlodipine/HCTZ). In a 12-week, randomized, double-blind, multicentre trial (TRINITY) in adults with moderate to severe hypertension, olmesartan medoxomil + amlodipine + HCTZ triple combination therapy produced significantly greater least squares mean reductions from baseline in seated diastolic blood pressure (BP) [primary endpoint] and seated systolic BP than olmesartan medoxomil/amlodipine, olmesartan medoxomil/HCTZ or amlodipine + HCTZ. Furthermore, significantly more patients achieved BP goals and targets with the triple combination regimen than with any of the dual combination regimens at week 12, with olmesartan medoxomil + amlodipine + HCTZ also demonstrating benefit over the dual regimens in terms of ambulatory BP control. According to subgroup analyses of the TRINITY trial, olmesartan medoxomil + amlodipine + HCTZ was more effective in reducing BP and achieving BP goals than each of the dual therapies, irrespective of hypertension severity, age, sex, race or diabetes mellitus status. Data from a number of smaller clinical studies indicated that olmesartan medoxomil + amlodipine + HCTZ triple combination therapy provides antihypertensive efficacy in patients whose BP is not adequately controlled with olmesartan medoxomil + amlodipine. Olmesartan medoxomil + amlodipine + HCTZ was generally well tolerated in the TRINITY study, with adverse events usually being mild or moderate in severity.
Topics: Amlodipine; Antihypertensive Agents; Drug Combinations; Humans; Hydrochlorothiazide; Hypertension; Imidazoles; Tetrazoles
PubMed: 21275446
DOI: 10.2165/11206770-000000000-00000 -
Drugs Dec 2010Olmesartan medoxomil is an orally administered angiotensin II receptor antagonist, selective for the angiotensin II type 1 receptor, which has established... (Review)
Review
Olmesartan medoxomil is an orally administered angiotensin II receptor antagonist, selective for the angiotensin II type 1 receptor, which has established antihypertensive efficacy in adults. In children and adolescents with hypertension (n = 302), oral olmesartan medoxomil significantly and dose-dependently reduced seated systolic blood pressure (BP) and seated dystolic BP from baseline (the primary endpoint) in a 3-week, dose-response period in a well designed phase II/III clinical trial. Patients received olmesartan medoxomil high dose (20 or 40 mg once daily depending on bodyweight) or low dose (2.5 or 5.0 mg once daily depending on bodyweight). The response was significant for both cohorts, which were stratified by race (cohort A was mixed race [62% White] and cohort B was 100% Black). In addition, BP control was maintained in olmesartan recipients relative to placebo recipients in cohort A and the combined cohort A + B, but not for patients in cohort B, during a placebo-controlled withdrawal period of this trial. Oral olmesartan medoxomil was generally well tolerated in children and adolescents with hypertension. The majority of adverse events were of mild to moderate intensity.
Topics: Adolescent; Angiotensin II Type 1 Receptor Blockers; Animals; Antihypertensive Agents; Child; Humans; Hypertension; Imidazoles; Olmesartan Medoxomil; Tetrazoles
PubMed: 21142262
DOI: 10.2165/11206310-000000000-00000 -
The Annals of Pharmacotherapy Jan 2003To review the pharmacology, pharmacokinetics, efficacy, and adverse effects of olmesartan medoxomil, an angiotensin II receptor antagonist for the treatment of... (Review)
Review
OBJECTIVE
To review the pharmacology, pharmacokinetics, efficacy, and adverse effects of olmesartan medoxomil, an angiotensin II receptor antagonist for the treatment of hypertension.
DATA SOURCES
Information was obtained from MEDLINE searches (1996-April 2002) of English-language medical literature. Search terms included CS-866, olmesartan, olmesartan medoxomil, RNH-6270 (active metabolite of olmesartan), Benicar, angiotensin receptors, and antihypertensive agents. In addition, references from relevant articles were reviewed for additional citations. The authors independently reviewed literature identified in the searches. Studies evaluating olmesartan (i.e., abstracts, clinical trials, data on file with manufacturer) were considered for inclusion.
STUDY SELECTION
All articles identified from data sources with pertinent information regarding olmesartan medoxomil were evaluated, and all information deemed relevant was included in this review.
DATA SYNTHESIS
Olmesartan medoxomil is a competitively priced addition to the class of angiotensin II receptor antagonists. Monotherapy with olmesartan medoxomil in once-daily doses of 20-40 mg has produced significant reductions in systolic and diastolic blood pressure in hypertensive patients. Adverse effects have been minimal with olmesartan medoxomil, with dizziness being the only adverse effect occurring more often than with placebo in clinical trials. Additionally, animal studies indicate that olmesartan medoxomil may prove to be useful treatment for diabetic nephropathy, as well as atherosclerosis.
CONCLUSIONS
Olmesartan medoxomil has a favorable safety and efficacy profile, with blood pressure-lowering effects comparable to those of other angiotensin receptor blockers (i.e., losartan, valsartan, irbesartan). At this time, formulary decisions will be driven primarily by economic issues. Theoretical benefits of olmesartan medoxomil in reducing atherogenesis and lowering angiotensin II concentrations better than the alternative agents will be determined only with more extensive research.
Topics: Angiotensin II; Angiotensin Receptor Antagonists; Antihypertensive Agents; Clinical Trials as Topic; Dose-Response Relationship, Drug; Drug Interactions; Humans; Hypertension; Imidazoles; Olmesartan Medoxomil; Prescription Fees; Receptors, Angiotensin; Tetrazoles
PubMed: 12503943
DOI: 10.1345/aph.1C197 -
Vascular Health and Risk Management 2006Olmesartan medoxomil is an angiotensin II receptor antagonist. In pooled analyses of seven randomized, double-blind trials, 8 weeks' treatment with olmesartan medoxomil... (Review)
Review
Olmesartan medoxomil is an angiotensin II receptor antagonist. In pooled analyses of seven randomized, double-blind trials, 8 weeks' treatment with olmesartan medoxomil was significantly more effective than placebo in terms of the response rate, proportion of patients achieving target blood pressure (BP) and mean change from baseline in diastolic (DBP) and systolic blood pressure (SBP). Olmesartan medoxomil had a fast onset of action, with significant between-group differences evident from 2 weeks onwards. The drug was well tolerated with a similar adverse event profile to placebo. In patients with type 2 diabetes, olmesartan medoxomil reduced renal vascular resistance, increased renal perfusion, and reduced oxidative stress. In several large, randomized, double-blind trials, olmesartan medoxomil 20 mg has been shown to be significantly more effective, in terms of primary endpoints, than recommended doses of losartan, valsartan, irbesartan, or candesartan cilexetil, and to provide better 24 h BP protection. Olmesartan medoxomil was at least as effective as amlodipine, felodipine and atenolol, and significantly more effective than captopril. The efficacy of olmesartan medoxomil in reducing cardiovascular risk beyond BP reduction is currently being investigated in trials involving patients at high risk due to atherosclerosis or type 2 diabetes.
Topics: Adrenergic beta-Antagonists; Angiotensin II Type 1 Receptor Blockers; Angiotensin-Converting Enzyme Inhibitors; Antihypertensive Agents; Blood Pressure; Calcium Channel Blockers; Cost-Benefit Analysis; Drug Costs; Humans; Hypertension; Imidazoles; Olmesartan Medoxomil; Randomized Controlled Trials as Topic; Research Design; Tetrazoles; Treatment Outcome
PubMed: 17323586
DOI: 10.2147/vhrm.2006.2.4.327 -
Clinical Therapeutics Apr 2003Regulation of the activity of the renin-angiotensin-aldosterone system has become important in the management of cardiovascular disease. Olmesartan medoxomil (CS-866) is... (Review)
Review
BACKGROUND
Regulation of the activity of the renin-angiotensin-aldosterone system has become important in the management of cardiovascular disease. Olmesartan medoxomil (CS-866) is the newest selective angiotensin II-receptor blocker (ARB) to be approved for the treatment of hypertension.
OBJECTIVE
This review describes the mechanism of action, pharmacokinetics, adverse-effect profile, drug-interaction potential, and dosing of olmesartan medoxomil. The results of relevant clinical efficacy and safety trials are also discussed.
METHODS
This review is based on data from published clinical efficacy and safety trials and abstracts of conference presentations. To identify appropriate English-language publications for review, MEDLINE (1966-October 2002) and EMBASE (1990-2002) were searched using the terms olmesartan medoxomil, CS-866, angiotensin II-receptor blocker, and hypertension.
RESULTS
Olmesartan medoxomil has been reported to be an effective agent for the treatment of hypertension. Its blood pressure-lowering effects were comparable to those of other antihypertensive agents and other ARBs. Effects were seen as early as 2 weeks and persisted when olmesartan medoxomil was administered long term (for 1 year). The maximum recommended daily dose is 40 mg, except in the presence of severe renal insufficiency (creatinine clearance <20 mL/min) or moderate hepatic insufficiency (Child-Pugh score 7-9), when the daily dose should not exceed 20 mg. Olmesartan medoxomil was well tolerated. The most commonly reported adverse effect occurring significantly more often with olmesartan medoxomil than with placebo was dizziness (seen in approximately 3% of patients). The occurrence of clinically significant drug interactions was minimal.
CONCLUSIONS
Based on the available literature, olmesartan medoxomil is an effective ARB for the treatment of hypertension, with a favorable adverse-effect and drug-interaction profile.
Topics: Angiotensin II; Angiotensin Receptor Antagonists; Antihypertensive Agents; Clinical Trials as Topic; Drug Interactions; Humans; Hypertension; Imidazoles; Olmesartan Medoxomil; Tetrazoles
PubMed: 12809956
DOI: 10.1016/s0149-2918(03)80066-8 -
Vascular Health and Risk Management 2006In most patients with hypertension, especially Stage 2 hypertension, adequate control of blood pressure (BP) is only achieved with combination drug therapy. When using... (Review)
Review
In most patients with hypertension, especially Stage 2 hypertension, adequate control of blood pressure (BP) is only achieved with combination drug therapy. When using combination therapy, antihypertensive agents with complementary mechanisms of action are recommended, for example, an angiotensin receptor blocker (ARB) in combination with hydrochlorothiazide (HCTZ), a beta-blocker + HCTZ, an ACE inhibitor + HCTZ, or a calcium channel blocker + an ACE inhibitor. One such combination is olmesartan medoxomil + HCTZ, which is available as fixed-dose, single-tablet combinations for once-daily administration. In clinical trials, olmesartan medoxomil/HCTZ reduced systolic BP (SBP) and diastolic BP (DBP) to a greater extent than either component as monotherapy. A clinical study in patients with Stage 1 or 2 hypertension showed that olmesartan medoxomil/HCTZ achieved a similar mean reduction in DBP, but a significantly greater mean reduction in SBP and higher rate of BP control (< 140/90 mmHg) than observed with losartan/HCTZ, at US/European-approved starting doses. In a non-inferiority trial, the antihypertensive efficacy of olmesartan medoxomil/HCTZ was comparable to that of atenolol/HCTZ. Furthermore, indirect comparisons have shown that olmesartan medoxomil/HCTZ compares favorably with other antihypertensive combination therapies, including other ARB/HCTZ combinations and amlodipine besylate/ benazepril. Olmesartan medoxomil/HCTZ is generally well tolerated. In conclusion, olmesartan medoxomil/HCTZ is an effective and well-tolerated combination antihypertensive therapy that results in significant BP reductions and BP control in many patients.
Topics: Angiotensin II Type 1 Receptor Blockers; Antihypertensive Agents; Blood Pressure; Diuretics; Drug Administration Schedule; Drug Combinations; Humans; Hydrochlorothiazide; Hypertension; Imidazoles; Olmesartan Medoxomil; Severity of Illness Index; Tetrazoles; Treatment Outcome
PubMed: 17323594
DOI: 10.2147/vhrm.2006.2.4.401 -
Vascular Health and Risk Management 2011Prevalence of hypertension in children and adolescents has progressively and continuously increased over recent decades. Thus, early and effective control of high blood... (Review)
Review
Prevalence of hypertension in children and adolescents has progressively and continuously increased over recent decades. Thus, early and effective control of high blood pressure may be considered an effective therapeutic approach, in order to reduce the burden of hypertension-related cardiovascular disease in future. In the past, due to the absence of prospective, long-term, randomized, controlled clinical trials performed in young hypertensive patients, lifestyle changes have been long seen as the only strategy to reduce high blood pressure levels. More recently, clinical data on the efficacy and safety of five major classes of antihypertensive drugs (including angiotensin converting enzyme inhibitors, angiotensin receptor blockers [ARBs], beta-blockers, calcium-antagonists, and diuretics) have become available. In particular, these trials demonstrated dose-dependent blood pressure reductions and a good tolerability profile of several ARBs in hypertensive children and adolescents. An overview is provided of the clinical benefits of early detection and prompt intervention of high blood pressure levels, with a closer analysis of recent clinical trials, performed with olmesartan medoxomil in young subjects with hypertension.
Topics: Adolescent; Angiotensin II Type 1 Receptor Blockers; Animals; Antihypertensive Agents; Blood Pressure; Child; Evidence-Based Medicine; Humans; Hypertension; Imidazoles; Olmesartan Medoxomil; Risk Assessment; Tetrazoles; Treatment Outcome
PubMed: 21490943
DOI: 10.2147/VHRM.S11672